Title (en)

NOVEL QUINUCLIDINE DERIVATIVE USEFUL IN THE PREPARATION OF MEQUITAZINE

Title (de)

NEUARTIGE CHINUCLIDINDERIVATE ZUR HERSTELLUNG VON MEQUITAZIN

Title (fr)

NOUVEAU DÉRIVE DE LA QUINUCLIDINE UTILE DANS LA PRÉPARATION DE LA MEQUITAZINE

Publication

EP 2109609 B1 20130612 (FR)

Application

EP 08761775 A 20080117

Priority

• FR 2008000056 W 20080117
• FR 0752742 A 20070118

Abstract (en)

[origin: FR2911606A1] 1-Aza-bicyclo-(2.2.2)-oct-2-en-3-ylmethyl acetate (I) is new. Also new is method for preparing mequitazine (II) from (I). 1-Aza-bicyclo-(2.2.2)-oct-2-en-3-ylmethyl acetate of formula (I) is new. Independent claims are included for: (1) a method for preparing mequitazine (II) from (I), involving (a) complexing (I) with palladium; (b) subjecting the product to allylic amination with phenothiazine to give dehydromequitazine (III); and (c) catalytically hydrogenating (III), preferably under enantio-selective conditions; and (2) the preparation of (I). ACTIVITY : Antiallergic. MECHANISM OF ACTION : Antihistamine.

IPC 8 full level

C07D 453/02 (2006.01)

CPC (source: EP US)

C07D 207/08 (2013.01 - EP US); C07D 211/26 (2013.01 - EP US); C07D 211/70 (2013.01 - EP US); C07D 279/26 (2013.01 - EP US); C07D 453/02 (2013.01 - EP US); C07D 471/04 (2013.01 - EP US)

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR

DOCDB simple family (publication)

FR 2911606 A1 20080725; FR 2911606 B1 20090417; AR 064966 A1 20090506; CA 2675118 A1 20080912; CA 2675118 C 20150217; EP 2109609 A1 20091021; EP 2109609 B1 20130612; JP 2010516663 A 20100520; JP 5174830 B2 20130403; US 2010105897 A1 20100429; US 2012088917 A1 20120412; US 8158784 B2 20120417; US 8304545 B2 20121106; WO 2008107545 A1 20080912

DOCDB simple family (application)

FR 0752742 A 20070118; AR P080100239 A 20080118; CA 2675118 A 20080117; EP 08761775 A 20080117; FR 2008000056 W 20080117; JP 2009545976 A 20080117; US 201113313809 A 20111207; US 52324908 A 20080117